Cat. No.: HY-120227

SM253

SM253 is an Hsp90 inhibitor that inhibits Hsp90-dependent protein folding. SM253 blocks chaperone function by binding to the N-middle linker region and the C-terminal M domain, reducing co-chaperone and client protein binding and activation. SM253 induces cancer cell apoptosis, activates caspase 3/7, causes cell cycle arrest and reduces cell proliferation, while decreasing Hsp90 client proteins such as AR, FKBP51, PSA, Cdk4, AKT, ERK, and p23, and reducing Hsp27/Hsp70 expression without inducing heat shock proteins. SM253 causes dose-dependent fibronectin loss in cells expressing LRP1. SM253 can be used for research on colon cancer, pancreatic cancer, and prostate cancer.

For research use only. We do not sell to patients.

CAS No.: 1610546-52-5
Formula: C₃₉H₅₂N₆O₅S
Molecular Weight:716.94

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

SM253 Chemical Structure

CAS No.: 1610546-52-5

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

^[1]^[2]

Caspase-3

Caspase-7

HSP90

HSP70

All HSP Isoforms :

All Caspase Isoforms :

All ERK Isoforms :

All Akt Isoforms :

All CDK Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
HCT-116	IC50	5.0 μM	Cytotoxicity against human HCT-116 colon carcinoma cells assessed as viability reduction by CCK8 assay. Cytotoxicity against human HCT-116 colon carcinoma cells assessed as viability reduction by CCK8 assay.	25050163
MIA PaCa-2	IC50	5.5 μM	Cytotoxicity against human MiaPaCa-2 pancreatic carcinoma cells assessed as viability reduction by CCK8 assay. Cytotoxicity against human MiaPaCa-2 pancreatic carcinoma cells assessed as viability reduction by CCK8 assay.	25050163
LNCaP	IC50	5.68 μM	Antiproliferative activity against human LNCaP prostate cancer cells assessed as growth inhibition after 4 days by viable cell count using Trypan blue dye exclusion. Antiproliferative activity against human LNCaP prostate cancer cells assessed as growth inhibition after 4 days by viable cell count using Trypan blue dye exclusion.	27526951
22Rv1	IC50	5.46 μM	Antiproliferative activity against human 22Rv1 prostate cancer cells assessed as growth inhibition after 4 days by viable cell count using Trypan blue dye exclusion. Antiproliferative activity against human 22Rv1 prostate cancer cells assessed as growth inhibition after 4 days by viable cell count using Trypan blue dye exclusion.	27526951
PC-3	IC50	7.31 μM	Antiproliferative activity against human PC-3 prostate cancer cells assessed as growth inhibition after 4 days by viable cell count using Trypan blue dye exclusion. Antiproliferative activity against human PC-3 prostate cancer cells assessed as growth inhibition after 4 days by viable cell count using Trypan blue dye exclusion.	27526951

In Vitro

Anti-cancerApoptosisCell Cycle RegulationOthers

Anti-cancer

The IC₅₀ values of SM253 in HCT-116 and MiaPaCa-2 cells are 5.0 μM and 5.5 μM, respectively^[1].
SM253 (2500-10000 nM; 4 days) inhibits the growth of LNCaP, 22Rv1, and PC-3 prostate cancer cells with an IC₅₀ of approximately 5 µM and reduces the proliferation of PC-3 cells^[2].
SM253 (5-10 μM; 48 h) reduces Hsp27/Hsp70 and selected Hsp90 client/co-chaperone proteins in LNCaP, 22Rv1, and PC-3 prostate cancer cells without inducing a heat shock response^[2].

Apoptosis

SM253 (50 μM; 24 h) induces apoptosis in HCT-116 and MiaPaCa-2 cells^[1].
SM253 (24 h) increases caspase 3/7 activity 4-fold in HCT-116 and MiaPaCa-2 cells^[1].
SM253 (5-10 μM; 48 h) induces caspase-dependent apoptosis in prostate cancer cell lines, and this cell death is blocked by the pan-caspase inhibitor Z-VAD-fmk (HY-16658B)^[2].

Cell Cycle Regulation

SM253 (24 h) arrests HCT-116 and MiaPaCa-2 cells in the G0/G1 phase^[1].

Others

SM253 (5 μM; 2 h) inhibits hsp90-mediated protein folding in rabbit reticulocyte lysate, reducing luciferase activity by 42%^[1].
SM253 (5-50 μM; 24 h) reduces HSR proteins by approximately 2-4 fold and depletes hsp27 in HCT-116 cells without inducing a heat shock response^[1].
SM253 (2-25 μM; 16 h) induces dose-dependent fibronectin loss in LRP1-expressing MEF-1 cells but not in LRP1-deficient PEA-13 cells^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Apoptosis Analysis^[1]

Cell Line:

HCT-116 and MiaPaCa-2 cells
Concentration:

50 μM
Incubation Time:

24 h
Result:

Induced apoptosis in 75% of cells.

Cell Viability Assay^[2]

Cell Line:

LNCaP, 22Rv1, and PC-3 human prostate cancer cell lines
Concentration:

2500, 5000, 10000 nM (growth/viability); 5 µM (IC₅₀; CFSE/Ki67); 10 µM (2×IC₅₀; CFSE/Ki67)
Incubation Time:

4 days (growth/viability); 48 h (Ki67)
Result:

Produced dose-dependent inhibition of cell growth in LNCaP, 22Rv1, and PC-3 cells with IC50 ~5 µM.
Reduced the percentage of actively proliferating LNCaP cells significantly in CFSE analysis.
Reduced Ki67 positivity significantly in PC-3 cells.
Did not produce statistically significant Ki67 reduction in LNCaP and 22Rv1 cells.

Apoptosis Analysis^[2]

Cell Line:

LNCaP, 22Rv1, and PC-3 human prostate cancer cell lines
Concentration:

5 and 10 μM
Incubation Time:

48 h
Result:

Displayed concentration-dependent cytotoxicity in prostate cancer cell lines.
Increased cleaved caspase-3 levels compared with vehicle-exposed control cells.
Prevented SM253-induced cell death with Z-VAD-fmk, confirming apoptosis.

Western Blot Analysis^[2]

Cell Line:

LNCaP, 22Rv1, and PC-3 human prostate cancer cell lines
Concentration:

5 and 10 μM
Incubation Time:

48 h
Result:

Decreased expression of Hsp27 and Hsp70 in LNCaP, 22Rv1, and PC-3 cells.
Reduced AR, FKBP51, PSA, Cdk4, AKT, ERK, FKBP52, and p23 dose-dependently in LNCaP cells.
Reduced Cdk4 and AKT expression and reduced p23 in 22Rv1 cells.
Caused a marked ≥2-fold decrease in HOP expression at 2×IC₅₀but did not affect FKBP52 in 22Rv1 cells.
Did not inhibit Cdk4 or ERK and reduced p23 in PC-3 cells.

Related Protocols :

Chemical Information

CAS No. 1610546-52-5
Molecular Weight 716.94
Formula C₃₉H₅₂N₆O₅S
SMILES

C([C@@H]1C(=O)N[C@H](CC2=CSC=N2)C(=O)N[C@H](CC(C)C)C(=O)N(C)[C@@H]([C@H](C)C)C(=O)N[C@@H](CC(C)C)C(=O)N1)(C3=CC=CC=C3)C4=CC=CC=C4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Koay YC, et al. Chemically accessible hsp90 inhibitor that does not induce a heat shock response. ACS medicinal chemistry letters. 2014 Jul 10;5(7):771-6.

[2]. Armstrong HK, et al. A Novel Class of Hsp90 C-Terminal Modulators Have Pre-Clinical Efficacy in Prostate Tumor Cells Without Induction of a Heat Shock Response. The Prostate. 2016 Dec;76(16):1546-1559.

[3]. Boel NM, et al. LRP1 is required for novobiocin-mediated fibronectin turnover. Scientific reports. 2018 Jul 30;8(1):11438.

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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SM253

All HSP Isoforms

All Caspase Isoforms

All ERK Isoforms

All Akt Isoforms

All CDK Isoforms